PKM2-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPKM2-IN-1Cat.No.:HY-103617CASNo.:94164-88-2分⼦式:C₁₈H₁₉NO₂S₂分⼦量:345.48作⽤靶点:PyruvateKinase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:320mg/mL(926.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8945mL14.4726mL28.9452mL5mM0.5789mL2.8945mL5.7890mL10mM0.2895mL1.4473mL2.8945mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:8mg/mL(23.16mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥8mg/mL(23.16mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥8mg/mL(23.16mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PKM2-IN-1⼀种丙酮酸激酶M2(PKM2)抑制剂，其IC50值为2.95μM。IC50&TargetIC50:2.95μM(PKM2)[1]体外研究PKM2-IN-1isapyruvatekinaseM2(PKM2)inhibitorwithanIC50of2.95±0.53μM.ResultsshowthatmostofthetestedcompoundsexhibitsomedegreeofPKM2inhibitionandsomecompounds,suchasPKM2-IN-1(compound3k)and6d,displaymorepotentactivitythanthepositivecontrolshikonin.TherepresentativecompoundsPKM2-IN-1,6ddisplaydose-dependentinhibitionofPKM2withlessinhibitionofPKM1andPKLlikeshikonin.Amongalltestedcompounds,themostpotentcompoundsare3a,PKM2-IN-1and3r,whichexhibitIC50valuesagainstHCT116andHelacellsrangingfrom0.39to0.41μM,0.18to0.29μMand0.18to0.38μM,respectively[1].PROTOCOLCellAssay[1]Celllines(HCT116,Hela,H1299,BEAS-2B)areculturedinRPMI1640containing9%fetalbovineserum(FBS)at37°Cin5%CO2.CellviabilityisdetectedwiththeMTSassayaccordingtothemanufacturer'sinstructions.Briefly,5000cellsinperwellareplatedin96-wellplates.Afterincubatedfor12h,thecellsaretreatedwithdifferentconcentrationoftestedcompound(includingPKM2-IN-1)orDMSO(asnegativecontrol)for48h.Then20μLMTSisaddedinperwellandincubatedat37°Cfor3h.Absorbanceofeachwellisdeterminedbyamicroplatereaderata490nmwavelength.TheIC50valuesarecalculatedusingPrismGraphpadsoftwareofthetriplicateexperiment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•SciAdv.2022Sep23;8(38):eabo0987.•EBioMedicine.2020Apr;54:102722.•CellRep.2022Mar8;38(10):110468.•JPathol.2022Apr;256(4):414-426.•EurJPharmacol.2019Apr17;854:232-239.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].NingX,etal.DiscoveryofnovelnaphthoquinonederivativesasinhibitorsofthetumorcellspecificM2isoformofpyruvatekinase.EurJMedChem.2017Sep29;138:343-352.McePdfHeightCaution:Producthasnotbeenfully